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TMX-2164

Names

[ CAS No. ]:
2418022-85-0

[ Name ]:
TMX-2164

Biological Activity

[Description]:

TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Bcl-2 Family
Research Areas >> Cancer

[Target]

IC50: 152 nM (BCL6)[1]


[In Vitro]

TMX-2164 (5 μM; 30 h; HEK293T-cells) displays sustained target engagement and to prolongs occupancy on BCL6 protein[1]. TMX-2164 (6.2 μM; 1, 3, and 5 d; SU-DHL-4 cells) exhibits single digit micromolar antiproliferative activity in SU-DHL-4 cells[1]. Cell Viability Assay[1] Cell Line: SU-DHL-4 cells Concentration: 6.2 μM Incubation Time: 1, 3, and 5 days Result: Inhibited cell growth with 5 days.

[References]

[1]. Teng M, et, al. Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface. ACS Med Chem Lett. 2020 Apr 3;11(6):1269-1273.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H24ClFN6O6S

[ Molecular Weight ]:
591.01


Related Compounds